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Method of treating atrophic vaginitis

a vaginitis and atrophic technology, applied in the field of triphenylethylene derivative compounds, can solve the problems of increasing the risk of uterine cancer four, affecting the health of women, and affecting the survival rate of women, so as to reduce the incidence of thrombogenic events, inhibit the proliferation of endometrial cells, and reduce the incidence of climacteric symptoms

Active Publication Date: 2017-06-13
KLAMERUS BERNADETTE +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a compound called triphenylethylene derivative, which is present in a therapeutically effective amount to produce tissue-specific estrogenic effects. This compound can reduce the risk of blood clotting, worsening of climacteric symptoms, and adverse uterine effects associated with unopposed triphenylethylene derivative administration during menopause.

Problems solved by technology

Itching, which often interferes with a restful sleep, is also due to thinning and inflammation of the vulvovaginal epithelial layer.
The removal of estrogen has a negative impact on a women's health, increasing the risk for osteoporosis and impeding urogenital health.
Tamoxifen stimulates uterine epithelial cell proliferation, increasing the risk of uterine cancer four-fold in women over 50 years of age, thus limiting its utility in treating healthy postmenopausal women (Fisher et al., J Natl Cancer Inst 1998; 90: 1371-88).
Overall, many women fear the increase risk of developing breast cancer with estrogen replacement therapy.
Thus, while estrogen therapy is effective in treating atrophic vaginitis, there is poor patient compliance.
Furthermore, there is no approved method for the treatment of atrophic vaginitis in breast cancer risk patients.
There is no approved vaginal administered method for the treatment of atrophic vaginitis with the use of triphenylethylene derivatives.
There is no approved vaginal administered method for the treatment of atrophic vaginitis with the use of triphenylethylene derivatives in combination with progesterone to be used in non-hysterectomized women.
Overall, a new method that would have the benefits of estrogens, and at the same time decrease the carcinogenic risks and side effects, is needed because the present methods are far from optimal.
No drug candidate has emerged to fill the needs of women who have increased carcinogenic risks and who require the benefits of estrogen replacement to live productive lives.

Method used

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  • Method of treating atrophic vaginitis
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Examples

Experimental program
Comparison scheme
Effect test

example 1

on of Triphenylethylene Derivative in Suppository Form

[0092]The present example provides a formulation of a pharmaceutical composition to treat symptoms associated with atrophic vaginitis. Table 3 summarizes the components and respective amounts of each component.

[0093]

TABLE 3Tamoxifen Citrate0.0200 gmSilica Gel0.0150 gmBase JAB: (fatty base)1.2485 gmSuppository Volume1.2835 gmCitric Acid 0.1% at 0.0013 gmFor pH Adjustment

example 2

on of Triphenylethylene Derivative in Cream Form

[0094]The present example provides a formulation of a pharmaceutical composition to treat symptoms associated with atrophic vaginitis. Table 4 summarizes the components and respective amounts of each component.

[0095]

TABLE 4Tamoxifen Citrate0.0200gmPropylene Glycol USP0.0333mlJC Base0.9467gm(Base B and Base M)Base B is emollient creamBase M is Vitamin E AcetateUSP Liquid (1 IU / mg)Total volume / per dose1.000gm

example 3

on of Triphenylethylene Derivative and Progesterone in Suppository Form

[0096]The present example provides a formulation of a pharmaceutical composition to treat symptoms associated with atrophic vaginitis. Table 5 summarizes the components and respective amounts of each component.

[0097]

TABLE 5Tamoxifen Citrate0.0200 gmProgesterone0.0300 gmSilica gel0.0150 gmBase JAB: (fatty base)1.2215 gmSuppository Volume1.2865 gmCitric Acid 0.1% at 0.0013 gmFor pH Adjustment

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PUM

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Abstract

The present invention provides novel pharmaceutical compositions containing triphenylethylene derivative compounds, and methods of using the composition for treatment of symptoms associated with atrophic vaginitis. The pharmaceutical compositions are prepared for the vaginal administration of triphenylethylene derivative compounds in single or combination therapies. Preferably, the triphenylethylene derivative is tamoxifen.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of and claims priority under 35 U.S.C. §120 to U.S. application Ser. No. 11 / 757,787, filed on Jun. 4, 2007, which claims priority under 35 U.S.C. §119, based on U.S. Provisional Application Ser. No. 60 / 810,715, filed Jun. 2, 2006, and 60 / 917,800, filed May 14, 2007, the disclosures of which are incorporated herein in their entirety.FIELD OF THE INVENTION[0002]The present invention relates to using triphenylethylene derivative compounds in a novel pharmaceutical composition for vaginal therapy for the treatment of symptoms associated with atrophic vaginitis.BACKGROUND OF THE INVENTION[0003]Atrophic vaginitis is a hormone-dependent disease involving the lower urinary tract, genital tract, and pelvic floor. Generally, atrophic vaginitis becomes evident during or after menopause, the symptoms increasing with age. Symptoms relating to urogenital aging are due to estrogen loss from follicular depletion in the ...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/02A61K47/02A61K47/14A61K31/56A61K9/00A61K31/57A61P5/24A61K47/22A61K31/215A61P15/02
CPCA61K9/0034A61K9/02A61K31/215A61K31/56A61K31/57A61K47/02A61K47/14A61K47/22A61K2300/00A61P15/02A61P29/00A61P43/00A61P5/24A61K31/138
Inventor KLAMERUS, BERNADETTECHOLLET, JANET A.MERMELSTEIN, FRED
Owner KLAMERUS BERNADETTE
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